Exploring bis-(indolyl)methane moiety as an alternative and innovative CAP group in the design of histone deacetylase (HDAC) inhibitors

  • Bioorg Med Chem Lett. 2009 May 15;19(10):2840-3. doi: 10.1016/j.bmcl.2009.03.101.
Giuseppe Giannini  1 ,  Mauro Marzi ,  Maria Di Marzo ,  Gianfranco Battistuzzi ,  Riccardo Pezzi ,  Tiziana Brunetti ,  Walter Cabri ,  Loredana Vesci ,  Claudio Pisano
Affiliations
PMID: 19359173 DOI: 10.1016/j.bmcl.2009.03.101
Abstract

In order to gather further knowledge about the structural requirements on histone deacetylase inhibitors (HDACi), starting from the schematic model of the common pharmacophore that characterizes this class of molecules (surface recognition CAP group-connection unit-linker region-Zinc Binding Group), we designed and synthesized a series of hydroxamic acids containing a bis-(indolyl)methane moiety. HDAC inhibition profile and antiproliferative activity were evaluated.